EP0072623A1 - Imidazole Fungicide - Google Patents
Imidazole Fungicide Download PDFInfo
- Publication number
- EP0072623A1 EP0072623A1 EP82303656A EP82303656A EP0072623A1 EP 0072623 A1 EP0072623 A1 EP 0072623A1 EP 82303656 A EP82303656 A EP 82303656A EP 82303656 A EP82303656 A EP 82303656A EP 0072623 A1 EP0072623 A1 EP 0072623A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- alkyl
- formula
- cycloalkyl
- compounds
- conh
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
- C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
- C07D295/033—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
Definitions
- the invention also provides a compound of the formula (I) or a pharmaceutically acceptable salt or pharmaceutical composition thereof for use in treating fungal infections (including prophylactic treatment) in animals including humans.
- the daily dosage level of the anti-fungal compounds of the formula (I) will be from 0.1 to 10 mg/kg (in divided doses) when administered by either the oral or parenteral route.
- tablets or capsules of the compounds can be expected to contain from 5 mg to 0.5 g of active compound for administration singly or two or more at a time as appropriate.
- the physician in any event will determine the actual dosage which will be most suitable for an individual patient and it will vary with the age, weight and response of the particular patient.
- the above dosages are exemplary of the average case. There can, of course, be individual instances where higher or lower dosage ranges are merited, and such are within the scope of this invention.
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB8122246 | 1981-07-18 | ||
GB8122246 | 1981-07-18 |
Publications (2)
Publication Number | Publication Date |
---|---|
EP0072623A1 true EP0072623A1 (fr) | 1983-02-23 |
EP0072623B1 EP0072623B1 (fr) | 1985-06-05 |
Family
ID=10523357
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP82303656A Expired EP0072623B1 (fr) | 1981-07-18 | 1982-07-13 | Imidazole Fungicide |
Country Status (7)
Country | Link |
---|---|
US (1) | US4435399A (fr) |
EP (1) | EP0072623B1 (fr) |
JP (1) | JPS5824567A (fr) |
DE (1) | DE3264036D1 (fr) |
DK (1) | DK321482A (fr) |
GR (1) | GR77222B (fr) |
IE (1) | IE53386B1 (fr) |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0150036A1 (fr) * | 1984-01-23 | 1985-07-31 | Hoechst Aktiengesellschaft | Dérivés de l'azolyl-aryl-alcanoles, procédés pour leur préparation et leur usage |
US4829065A (en) * | 1987-04-24 | 1989-05-09 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US4935417A (en) * | 1987-04-24 | 1990-06-19 | Syntex Pharmaceuticals Ltd. | Sustituted imidazolyl-alkyl-piperazine and -diazepine derivatives for treating cerebrovascular disease |
US4973591A (en) * | 1988-10-21 | 1990-11-27 | Syntex Pharmaceuticals, Ltd. | Parenteral formulations of 1-diphenylmethyl-4-((2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl)piperazine |
US5010075A (en) * | 1987-04-24 | 1991-04-23 | Syntex Pharmaceuticals Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5043447A (en) * | 1987-04-24 | 1991-08-27 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5063220A (en) * | 1988-10-21 | 1991-11-05 | Syntex Pharmaceuticals, Ltd. | Parenteral formulations of 1-diphenylmethyl-4-((2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl)piperazine |
US5091428A (en) * | 1987-04-24 | 1992-02-25 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5142052A (en) * | 1988-04-22 | 1992-08-25 | Laboratoires Syntex | Cationic effect-driven carbinol/amine reaction |
US5252736A (en) * | 1987-04-24 | 1993-10-12 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
WO2000008006A2 (fr) * | 1998-08-07 | 2000-02-17 | Eli Lilly And Company Limited | Composes pharmaceutiques |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0001654A1 (fr) * | 1977-10-13 | 1979-05-02 | Siegfried Aktiengesellschaft | Dérivés d'imidazolyléthylène-oxyalcoyloxy et leurs analogues thio, leurs procédés de préparation et compositions pharmaceutiques les contenant |
EP0019190A2 (fr) * | 1979-05-19 | 1980-11-26 | Bayer Ag | Utilisation des hydroxyalkyl-imidazoles comme fongicides |
EP0023103A1 (fr) * | 1979-07-04 | 1981-01-28 | Pfizer Limited | Dérivés d'imidazole à activité antifongique, procédé pour leur préparation et leurs compositions pharmaceutiques |
EP0040345A1 (fr) * | 1980-05-16 | 1981-11-25 | Bayer Ag | Dérivés de 1-hydroxyéthyl-azoles, procédé pour leur préparation et leur utilisation comme fongicides et pour la régulation de la croissance des plantes |
-
1982
- 1982-06-25 US US06/392,394 patent/US4435399A/en not_active Expired - Fee Related
- 1982-07-13 DE DE8282303656T patent/DE3264036D1/de not_active Expired
- 1982-07-13 EP EP82303656A patent/EP0072623B1/fr not_active Expired
- 1982-07-15 GR GR68777A patent/GR77222B/el unknown
- 1982-07-16 DK DK321482A patent/DK321482A/da not_active Application Discontinuation
- 1982-07-16 IE IE1721/82A patent/IE53386B1/en unknown
- 1982-07-19 JP JP57125588A patent/JPS5824567A/ja active Granted
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0001654A1 (fr) * | 1977-10-13 | 1979-05-02 | Siegfried Aktiengesellschaft | Dérivés d'imidazolyléthylène-oxyalcoyloxy et leurs analogues thio, leurs procédés de préparation et compositions pharmaceutiques les contenant |
EP0019190A2 (fr) * | 1979-05-19 | 1980-11-26 | Bayer Ag | Utilisation des hydroxyalkyl-imidazoles comme fongicides |
EP0023103A1 (fr) * | 1979-07-04 | 1981-01-28 | Pfizer Limited | Dérivés d'imidazole à activité antifongique, procédé pour leur préparation et leurs compositions pharmaceutiques |
EP0040345A1 (fr) * | 1980-05-16 | 1981-11-25 | Bayer Ag | Dérivés de 1-hydroxyéthyl-azoles, procédé pour leur préparation et leur utilisation comme fongicides et pour la régulation de la croissance des plantes |
Cited By (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0150036A1 (fr) * | 1984-01-23 | 1985-07-31 | Hoechst Aktiengesellschaft | Dérivés de l'azolyl-aryl-alcanoles, procédés pour leur préparation et leur usage |
US5252736A (en) * | 1987-04-24 | 1993-10-12 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US4829065A (en) * | 1987-04-24 | 1989-05-09 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US4935417A (en) * | 1987-04-24 | 1990-06-19 | Syntex Pharmaceuticals Ltd. | Sustituted imidazolyl-alkyl-piperazine and -diazepine derivatives for treating cerebrovascular disease |
US5010075A (en) * | 1987-04-24 | 1991-04-23 | Syntex Pharmaceuticals Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5043447A (en) * | 1987-04-24 | 1991-08-27 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5276034A (en) * | 1987-04-24 | 1994-01-04 | Syntex Pharmaceutical Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5091428A (en) * | 1987-04-24 | 1992-02-25 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
US5142052A (en) * | 1988-04-22 | 1992-08-25 | Laboratoires Syntex | Cationic effect-driven carbinol/amine reaction |
US4973591A (en) * | 1988-10-21 | 1990-11-27 | Syntex Pharmaceuticals, Ltd. | Parenteral formulations of 1-diphenylmethyl-4-((2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl)piperazine |
US5063220A (en) * | 1988-10-21 | 1991-11-05 | Syntex Pharmaceuticals, Ltd. | Parenteral formulations of 1-diphenylmethyl-4-((2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl)piperazine |
WO2000008006A2 (fr) * | 1998-08-07 | 2000-02-17 | Eli Lilly And Company Limited | Composes pharmaceutiques |
WO2000008006A3 (fr) * | 1998-08-07 | 2000-08-03 | Lilly Co Eli | Composes pharmaceutiques |
Also Published As
Publication number | Publication date |
---|---|
DE3264036D1 (en) | 1985-07-11 |
JPS6121630B2 (fr) | 1986-05-28 |
GR77222B (fr) | 1984-09-11 |
IE53386B1 (en) | 1988-10-26 |
JPS5824567A (ja) | 1983-02-14 |
EP0072623B1 (fr) | 1985-06-05 |
DK321482A (da) | 1983-01-19 |
US4435399A (en) | 1984-03-06 |
IE821721L (en) | 1983-01-18 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
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17P | Request for examination filed |
Effective date: 19820716 |
|
AK | Designated contracting states |
Designated state(s): AT BE CH DE FR GB IT LI LU NL SE |
|
ITF | It: translation for a ep patent filed |
Owner name: MODIANO & ASSOCIATI S.R.L. |
|
RBV | Designated contracting states (corrected) |
Designated state(s): BE DE FR GB IT LU NL |
|
GRAA | (expected) grant |
Free format text: ORIGINAL CODE: 0009210 |
|
RAP1 | Party data changed (applicant data changed or rights of an application transferred) |
Owner name: PFIZER CORPORATION Owner name: PFIZER LIMITED |
|
AK | Designated contracting states |
Designated state(s): BE DE FR GB IT LU NL |
|
REF | Corresponds to: |
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STAA | Information on the status of an ep patent application or granted ep patent |
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